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telapristone acetate

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telapristone acetate

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Telapristone (), as telapristone acetate (proposed brand names Proellex, Progenta; former code name CDB-4124), is a synthetic, steroidal selective progesterone receptor modulator (SPRM) related to mifepristone which is under development by Repros Therapeutics for the treatment of breast cancer, endometriosis, and uterine fibroids. It was originally developed by the National Institutes of Health (NIH), and, as of 2017, is in phase II clinical trials for the aforementioned indications. In addition to its activity as an SPRM, the drug also has some antiglucocorticoid activity.

Chemical data

Formula
C31H39NO5
Molecular weight
505.6 g/mol
IUPAC name
[(8S,11R,13S,14S,17R)-11-[4-(dimethylamino)phenyl]-17-(2-methoxyacetyl)-13-methyl-3-oxo-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-17-yl] acetate
SMILES
CC(=O)O[C@@]1(CC[C@@H]2[C@@]1(C[C@@H](C3=C4CCC(=O)C=C4CC[C@@H]23)C5=CC=C(C=C5)N(C)C)C)C(=O)COC
InChIKey
JVBGZFRPTRKSBB-MJBQOYBXSA-N
XLogP
3.4
Polar surface area
72.9 Ų
H-bond donors
0
H-bond acceptors
6
Formal charge
0

via PubChem

Drug data · ChEMBL

Max clinical phase
Phase 3
Molecule type
Small molecule
Indications
uterine fibroid, endometriosis, liver disease, kidney disease

via ChEMBL · EBI

Wikidata facts

Mass
505.283
Show 3 more facts
chemical formula
C₃₁H₃₉NO₅
canonical SMILES
CC(=O)OC1(CCC2C1(CC(C3=C4CCC(=O)C=C4CCC23)C5=CC=C(C=C5)N(C)C)C)C(=O)COC
isomeric SMILES
CC(=O)O[C@@]1(CC[C@@H]2[C@@]1(C[C@@H](C3=C4CCC(=O)C=C4CC[C@@H]23)C5=CC=C(C=C5)N(C)C)C)C(=O)COC
Sources (2)

via Wikidata · CC0

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Encyclopedic overview

3 sections
Contents
  • See also
  • References
  • External links

Telapristone (), as telapristone acetate (proposed brand names Proellex, Progenta; former code name CDB-4124), is a synthetic, steroidal selective progesterone receptor modulator (SPRM) related to mifepristone which is under development by Repros Therapeutics for the treatment of breast cancer, endometriosis, and uterine fibroids. It was originally developed by the National Institutes of Health (NIH), and, as of 2017, is in phase II clinical trials for the aforementioned indications. In addition to its activity as an SPRM, the drug also has some antiglucocorticoid activity.

==See also== List of investigational sex-hormonal agents § Progestogenics Aglepristone Lilopristone Onapristone Toripristone

Excerpted from Wikipedia’s “telapristone acetate” article, available under the CC BY-SA 4.0 licence.

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